Econazole-pharmex

INSTRUCTIONS for medical use of the medicinal product ECONAZOLE-PHARMEX (ECONAZOLE-PHARMEX)

Composition:

Active substance: econazole;

1 pessary contains 150 mg of econazole nitrate (calculated as 100% dry substance);

Excipient: hard fat.

Dosage form. Pessaries.

Main physicochemical characteristics: smooth pessaries of white or almost white color, torpedo-shaped. On longitudinal section, absence of specks is observed; presence of a cup-shaped depression and an air channel is permitted.

Pharmacotherapeutic group. Antimicrobial and antiseptic agents used in gynecology. ATC code G01AF05.

Pharmacological properties.

Pharmacodynamics.

The drug is a triazole fungicide. It exhibits antifungal activity against dermatophytes, yeasts, and molds. It is active against certain Gram-positive and Gram-negative bacteria. The action of econazole nitrate involves damaging fungal cell membranes by increasing fungal cell permeability and damaging intracellular membranes in the cytoplasm. The site of action is likely the acyl residues of unsaturated fatty acids in membrane phospholipids.

Pharmacokinetics.

After vaginal administration, econazole nitrate is absorbed to a negligible extent.

Maximum concentrations of econazole and/or its metabolites were observed within 1–2 days after administration and amounted to 65 ng/mL.

Econazole and/or its metabolites in systemic circulation are predominantly bound to serum proteins (> 98%). Econazole is mainly metabolized via oxidation, deamination and/or O-dealkylation; its metabolites are excreted in urine and feces.

Clinical characteristics.

Indications.

Vulvovaginal fungal infections caused by pathogens sensitive to econazole.

Contraindications.

Hypersensitivity to any component of the drug.

Interaction with other medicinal products and other forms of interaction.

Econazole-Pharmex should not be used concomitantly with other gynecological medicinal products for intravaginal or topical use based on mineral oil, vegetable oil, or vaseline.

Appropriate studies have not been conducted. Since econazole is chemically similar to imidazole derivatives, there is a possibility of competitive interaction between econazole nitrate and substances metabolized by CYP3A/2C29 enzymes. However, due to the low systemic absorption of the drug, the occurrence of clinically significant interactions is unlikely.

Patients taking oral anticoagulants such as warfarin, acenocoumarol, and phenprocoumon should exercise caution and monitor blood coagulation parameters. Dosage adjustment of oral anticoagulants may be required during and after treatment with econazole.

Concomitant use of diaphragms or condoms with Econazole-Pharmex should be avoided. Such interaction may reduce the efficacy of the medicinal product and weaken the integrity of barrier contraceptives.

Special precautions for use.

Econazole-Pharmes is intended for vaginal use only and should not be administered orally. The suppositories should be placed in a cool place 30 minutes before administration.

Econazole-Pharmes suppositories contain a fatty base which may damage rubber contraceptives such as diaphragms or latex condoms and reduce their effectiveness; therefore, the use of these contraceptive methods should not be combined with this medication. Patients using spermicidal contraceptives should consult their physician, as local vaginal treatment may inactivate the action of spermicidal contraceptives.

Econazole-Pharmes should not be used in combination with other gynecological medications prescribed by a physician for oral or topical use.

If symptoms of irritation or hypersensitivity occur, treatment should be discontinued.

Patients who are hypersensitive to imidazole-group drugs may also exhibit hypersensitivity to econazole nitrate.

The efficacy and safety of use in women over 65 years of age have not been established.

Use during pregnancy or breastfeeding.

Pregnancy

Animal studies have shown that econazole nitrate has no teratogenic effects; however, fetotoxicity was observed at high doses. The significance of these findings for humans is unknown.

The drug is absorbed systemically from the vagina; therefore, it should not be used during the first trimester of pregnancy unless the physician determines that treatment with this medication is essential for the patient's health. During the second and third trimesters of pregnancy, Econazole-Pharmes may be used if the potential benefit to the mother outweighs the possible risk to the fetus.

Breastfeeding

It is unknown whether econazole nitrate is excreted in human breast milk; therefore, during breastfeeding, the drug should be used with caution, considering the benefit-risk balance.

Ability to affect reaction speed when driving or operating machinery.

Econazole does not affect reaction speed when driving or operating machinery.

Method of Administration and Dosage

For adults, insert 1 suppository into the posterior vaginal fornix once daily at bedtime, preferably while lying on the back. The treatment course is 3 consecutive days. In case of recurrence or if culture analysis is positive one week after treatment, a repeat course of treatment should be administered.

Children

The safety and efficacy of the drug in children have not been established.

Overdose

Adverse reactions expected in case of overdose are likely to be similar to the general profile of adverse reactions.

Cases of overdose have not been reported.

In case of accidental oral ingestion, nausea, vomiting, and diarrhea may occur. In such cases, symptomatic therapy should be administered as needed.

Econazole-Pharmex is intended for vaginal use. In case of accidental ingestion, symptomatic treatment should be carried out. If the drug comes into contact with the eyes, they should be immediately flushed with water or physiological saline solution. If irritation symptoms persist, medical advice should be sought.

Adverse Reactions

Immune system disorders: hypersensitivity.

Skin and subcutaneous tissue disorders: pruritus, skin burning sensation, rash, erythema, angioedema, urticaria, contact dermatitis, skin desquamation.

Reproductive system and breast disorders: vaginal burning sensation.

General disorders and administration site conditions: application site pain, application site irritation, application site swelling.

Note: angioedema, erythema, urticaria, hypersensitivity, contact dermatitis, skin desquamation, application site pain, application site irritation, and application site swelling are listed according to the Medical Dictionary for Regulatory Activities (MedDRA), version 13.0. Other adverse reactions are listed according to MedDRA version 12.0.

Shelf life: 3 years.

Storage conditions:

Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging:

3 suppositories per blister, 1 blister per carton; 5 suppositories per blister, 1 or 2 blisters per carton.

Prescription status: Prescription only.

Manufacturer: LLC "FARMEKS GROUP".

Manufacturer's address:

100, Shevchenka Street, city of Boryspil, Kyiv region, 08301, Ukraine.

All cases of adverse reactions should be reported to the manufacturer:

LLC "Farmeks Group", Ukraine, 08301, Kyiv region, city of Boryspil, Shevchenka Street, 100, tel: +38(044)391-19-19, fax: +38(044)391-19-18, or via the form on the website: http://www.pharmex.com.ua/kontakty/farmakonadzor